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1. 发明申请

WO1996023769A2 HETEROCYCLIC COMPOUNDS POSSESSING 5HT2C RECEPTOR ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有5HT2C受体拮抗剂活性的杂环化合物
公开(公告)号：WO1996023769A2
公开(公告)日：1996-08-08
申请号：PCT/EP1996000369
申请日：1996-01-24
申请人： SMITHKLINE BEECHAM PLC , GASTER, Laramie, Mary , WYMAN, Paul, Adrian , MULHOLLAND, Keith, Raymond , DAVIES, David, Thomas
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D209/08
CPC分类号： C07D409/12 , C07D209/08
摘要： The invention relates to heterocyclic families of compounds having pharmacological activity, in particular possessing 5HT2C receptor antagonist activity processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders.
摘要翻译：本发明涉及具有药理学活性的化合物的杂环族，特别是其具有5HT 2C受体拮抗剂活性的制备方法，含有它们的组合物及其在治疗CNS病症中的用途。

2. 发明申请

WO1996023783A1 INDOLE DERIVATIVES AS 5-HT RECEPTOR ANTAGONIST 审中-公开
标题翻译：作为5-HT受体拮抗剂的吲哚衍生物
公开(公告)号：WO1996023783A1
公开(公告)日：1996-08-08
申请号：PCT/EP1996000368
申请日：1996-01-26
申请人： SMITHKLINE BEECHAM PLC , GASTER, Laramie, Mary , WYMAN, Paul, Adrian , MULHOLLAND, Keith, Raymond , DAVIES, David, Thomas , DUCKWORTH, David, Malcom , FORBES, Ian, Thomson , JONES, Graham, Elgin
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/14
摘要： The invention relates to heterocyclic compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders such as anxiety.
摘要翻译：本发明涉及具有药理活性的杂环化合物，其制备方法，含有它们的组合物及其在治疗CNS疾病如焦虑症中的用途。

3. 发明申请

WO1995006644A1 AMIDE DERIVATIVES AS 5HT1D RECEPTOR ANTAGONISTS 审中-公开
标题翻译： AMT衍生物作为5HT1D受体拮抗剂
公开(公告)号：WO1995006644A1
公开(公告)日：1995-03-09
申请号：PCT/EP1994002661
申请日：1994-08-09
申请人： SMITHKLINE BEECHAM PLC , DUCKWORTH, David, Malcolm , GASTER, Laramie, Mary , MULHOLLAND, Keith, Raymond , WYMAN, Paul, Adrian
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D295/14
CPC分类号： C07D213/40 , C07C2601/14 , C07D271/06 , C07D295/155
摘要： Novel amide derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments are disclosed.
摘要翻译：公开了新型酰胺衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。

4. 发明申请

WO1994008965A1 N-ALKYLPIPERIDINYL-4-METHYL CARBOXYLIC ESTERS/AMIDES OF CONDENSED RING SYSTEMS AS 5-HT4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为5-HT4受体拮抗剂的缩合环系的N-烷基哌啶-4-基甲基羧酸酯/氨基酸
公开(公告)号：WO1994008965A1
公开(公告)日：1994-04-28
申请号：PCT/GB1993002130
申请日：1993-10-14
申请人： SMITHKLINE BEECHAM PLC , GASTER, Laramie, Mary , JOINER, Graham, Francis , MULHOLLAND, Keith, Raymond , WYMAN, Paul, Adrian
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D211/22
CPC分类号： C07D401/12 , C07D211/22 , C07D405/12 , C07D413/12
摘要： Compounds of formula (I), wherein formula (I) consists of formulae (I-1) to (I-5), and pharmaceutically acceptable salts thereof, and the use of compound of formula (I) or a pharmaceutically acceptable salt thereof and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
摘要翻译：式（I）化合物，其中式（I）由式（I-1）至（I-5）组成，及其药学上可接受的盐，以及式（I）化合物或其药学上可接受的盐和它们作为药物用于治疗胃肠道疾病，心血管疾病和CNS疾病。

5. 发明申请

WO1993005038A1 5-HT4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 5-HT4受体拮抗剂
公开(公告)号：WO1993005038A1
公开(公告)日：1993-03-18
申请号：PCT/GB1992001649
申请日：1992-09-09
申请人： SMITHKLINE BEECHAM PLC , KING, Francis, David , GASTER, Laramie, Mary , MULHOLLAND, Keith, Raymond , RAHMAN, Shirley, Katherine , WYMAN, Paul, Adrian , SANGER, Gareth, John , WARDLE, Kay, Alison , BAXTER, Gordon, Smith , KENNETT, Guy, Anthony , KAUMANN, Alberto, Julio
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D405/12
CPC分类号： C07D405/12 , A61K31/245 , A61K31/38 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/437 , A61K31/445 , A61K31/4453 , A61K31/452 , A61K31/454 , A61K31/47 , A61K31/55 , C07D209/42 , C07D409/12 , C07D413/04 , C07D413/10 , C07D455/02 , C07D471/04
摘要： The use of a compound of formula (I) or pharmaceutically acceptable salt thereof, in which X1-(CH2)x-X2 forms a 5-7 membered ring wherein: X1 is O or S; X2 is O, S, NR or NRCO wherein R is hydrogen or C1-6alkyl; x is 1, 2 or 3; Y is O or NH; Z is sub-formula (a), (b) or (c) in the manufacture of a medicament for use in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
摘要翻译：使用式（I）化合物或其药学上可接受的盐，其中X 1 - （CH 2）x -X 2形成5-7元环，其中：X 1是O或S; X 2是O，S，NR或NRCO，其中R是氢或C 1-6烷基; x为1,2或3; Y是O或NH; Z是在制备用于治疗胃肠疾病，心血管疾病和CNS障碍的药物中的子式（a），（b）或（c）。

6. 发明申请

WO1994027987A1 5-HT4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 5-HT4受体拮抗剂
公开(公告)号：WO1994027987A1
公开(公告)日：1994-12-08
申请号：PCT/EP1994001583
申请日：1994-05-16
申请人： SMITHKLINE BEECHAM PLC , KING, David, Francis , GASTER, Laramie, Mary , MULHOLLAND, Keith, Raymond
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D401/06
CPC分类号： C07D401/06
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of the formula (I): X-CO-CH2-Z, or a pharmaceutically acceptable salt thereof, wherein X is a monocyclic or polycyclic aromatic group, Z is of sub-formula (h), (j) or (k), wherein n is 1, 2, 3 or 4; n is 0, 1, 2, 3 or 4; n is 2, 3, 4 or 5; q is 0, 1, 2 or 3; p is 0, 1 or 2; m is 0, 1 or 2; R is hydrogen, C1-12 alkyl, aralkyl or R5 is (CH2)z-R10 wherein z is 2 or 3 and R10 is selected from cyano, hydroxyl, C1-6 alkoxy, phenoxy, C(O)C1-6 alkyl, COC6H5, -CONR11R12, NR11COR12, SO2NR11R12 or NR11SO2R12 wherein R11 and R12 are hydrogen or C1-6 alkyl; or R5 is straight or branched chain alkylene of chain length 1-6 carbon atoms terminally substituted by aryl, 3 to 8 membered cycloalkyl, 3 to 8 membered heterocyclyl, 5 or 6 membered monocyclic heteroaryl or 9 or 10 membered fused bicyclic heteroaryl linked through carbon, C2-7 alkoxycarbonyl, or secondary or tertiary hydroxy substituted C1-6 alkyl; and R6, R7 and R8 are independently hydrogen or C1-6 alkyl; and R9 is hydrogen or C1-10 alkyl; and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
摘要翻译：式（I）化合物及其药学上可接受的盐，以及式（I）化合物：X-CO-CH 2 -Z或其药学上可接受的盐的用途，其中X是单环或多环芳基， Z为亚式（h），（j）或（k），其中n 1为1,2,3或4; n 2是0，1，2，3或4; n 3为2,3,4或5; q为0,1,2或3; p为0,1或2; m为0,1或2; R 5是氢，C 1-12烷基，芳烷基或R 5是（CH 2）z -R 10，其中z是2或3，R 10选自氰基，羟基，C 1-6烷氧基，苯氧基，C（O） C6烷基，COC6H5，-CONR11R12，NR11COR12，SO2NR11R12或NR11SO2R12，其中R11和R12是氢或C1-6烷基; 或R5是由芳基末端取代的链长1-6个碳原子的直链或支链亚烷基，3至8元环烷基，3至8元杂环基，5或6元单环杂芳基或通过碳键连接的9或10元稠合双环杂芳基，C 2-7烷氧基羰基，或仲或叔羟基取代的C 1-6烷基; 且R 6，R 7和R 8独立地为氢或C 1-6烷基; 并且R 9为氢或C 1-10烷基; 以及它们作为药物用于治疗胃肠道疾病，心血管疾病和CNS疾病的用途。

7. 发明申请

WO1994008994A1 HETEROCYCLIC -ESTERS OR -AMIDES USED AS 5-HT4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为5-HT4受体拮抗剂使用的杂环化合物或其衍生物
公开(公告)号：WO1994008994A1
公开(公告)日：1994-04-28
申请号：PCT/EP1993002775
申请日：1993-10-08
申请人： SMITHKLINE BEECHAM PLC , KING, Francis, David , GASTER, Laramie, Mary , JOINER, Graham, Francis , MULHOLLAND, Keith, Raymond , RAHMAN, Shirley, Katherine
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D405/12
CPC分类号： C07D401/12 , C07D405/12 , C07D409/12 , C07D455/02
摘要： Compounds of formula (I), wherein formula (I) consists of formulae (I-1) to (I-4), and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof, and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorder.
摘要翻译：式（I）化合物，其中式（I）由式（I-1）至（I-4）组成，及其药学上可接受的盐，以及式（I）化合物或其药学上可接受的盐，以及它们作为药物用于治疗胃肠道疾病，心血管疾病和CNS障碍的用途。

8. 发明申请

WO1994005654A1 HETEROARYL COMPOUNDS USED AS PHARMACEUTICALS 审中-公开
标题翻译：用作药物的异氟烷化合物
公开(公告)号：WO1994005654A1
公开(公告)日：1994-03-17
申请号：PCT/GB1993001895
申请日：1993-09-07
申请人： SMITHKLINE BEECHAM PLC , KING, Francis, David , GASTER, Laramie, Mary , MULHOLLAND, Keith, Raymond
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D405/12
CPC分类号： C07D405/12
摘要： Compounds of formula (I) for use in the treatment or prophylaxis of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
摘要翻译：用于治疗或预防胃肠道疾病，心血管疾病和CNS疾病的式（I）化合物。

9. 发明申请

WO1995006044A1 AMIDE AND UREA DERIVATIVES AS 5HT1D RECEPTOR ANTAGONISTS 审中-公开
标题翻译： AMHT和UREA衍生物作为5HT1D受体拮抗剂
公开(公告)号：WO1995006044A1
公开(公告)日：1995-03-02
申请号：PCT/EP1994002662
申请日：1994-08-09
申请人： SMITHKLINE BEECHAM PLC , DUCKWORTH, David, Malcolm , GASTER, Laramie, Mary , JENKINS, Sarah, Margaret , JENNINGS, Andrew, John , MULHOLLAND, Keith, Raymond
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D295/12
CPC分类号： C07D213/40 , C07D213/56 , C07D295/135 , C07D333/38
摘要： Novel amide and urea derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments are disclosed.
摘要翻译：公开了新型酰胺和脲衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。

10. 发明申请

WO1994008995A1 HETEROCYCLIC CONDENSED BENZOIC ACID DERIVATIVES AS 5-HT4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为5-HT4受体拮抗剂的杂环稠合苯甲酸衍生物
公开(公告)号：WO1994008995A1
公开(公告)日：1994-04-28
申请号：PCT/EP1993002809
申请日：1993-10-12
申请人： SMITHKLINE BEECHAM PLC , GASTER, Laramie, Mary , MULHOLLAND, Keith, Raymond
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D405/12
CPC分类号： C07D405/12 , C07D409/12 , C07D413/12
摘要： Compounds of formula (I), wherein formula (I) consists of formulae (I-1) to (I-4), and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof, (I-1), (I-2), (I-3), (I-4) and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders. The compounds are 5-HT4 receptor antagonists.
摘要翻译：式（I）化合物，其中式（I）由式（I-1）至（I-4）组成，及其药学上可接受的盐，以及式（I）化合物或其药学上可接受的盐，（I-1），（I-2），（I-3），（I-4）及其作为药物用于治疗胃肠道疾病，心血管疾病和CNS障碍的用途。该化合物是5-HT 4受体拮抗剂。

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